AR056684A1 - Derivados de acil-indol, composiciones farmaceuticas que los contienen y su uso en el tratamiento de la diabetes mellitus tipo 2. - Google Patents

Derivados de acil-indol, composiciones farmaceuticas que los contienen y su uso en el tratamiento de la diabetes mellitus tipo 2.

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Publication number
AR056684A1
AR056684A1 ARP060104426A ARP060104426A AR056684A1 AR 056684 A1 AR056684 A1 AR 056684A1 AR P060104426 A ARP060104426 A AR P060104426A AR P060104426 A ARP060104426 A AR P060104426A AR 056684 A1 AR056684 A1 AR 056684A1
Authority
AR
Argentina
Prior art keywords
alkyl
groups
halo
optionally substituted
alkoxy
Prior art date
Application number
ARP060104426A
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English (en)
Original Assignee
Merck & Co Inc
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Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR056684A1 publication Critical patent/AR056684A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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

Abstract

Indoles sustituidos y composiciones farmacéuticas que contienen dichos compuestos. Los compuestos son antagonistas del receptor de glucagon y por lo tanto son utiles para tratar, prevenir o retrasar la aparicion de diabetes mellitus de tipo 2 y afecciones relacionadas. Reivindicacion 1: Un compuesto representado por la formula (1) o una sal o solvato farmacéuticamente aceptable del mismo, en el que: cada R1 representa H o se selecciona independientemente entre el grupo constituido por: a) OH, halo, CO2Ra, C(O)NRbRc, NRbRc, CN o S(O)pRd; y b) alquilo C1-10, alquenilo C2-10, O-alquilo C1-10 y O-alquenilo C3-10, estando dichos grupos opcionalmente sustituidos con: (1) 1-5 grupos halo hasta un grupo perhaloalquilo; (2) 1 grupo oxo; (3) 1- 2 grupos OH; (4) 1 anillo fenilo, que está opcionalmente sustituido de la siguiente manera: 1-5 grupos halo hasta perhalo; 1-3 grupos alquilo o alcoxi C1-10, estando además cada uno opcionalmente sustituido con 1-5 halo hasta perhalo; R2 representa H o se selecciona entre el grupo constituido por: a) alquilo C1-14 o alquenilo C2-10, estando dichos grupos alquilo y alquenilo opcionalmente sustituidos con 1-5 átomos de halo hasta perhalo; 1-2 grupos OH, S(O)pRd, alcoxi C1-6 o halo-alcoxi C1-6; y 1-2 grupos arilo, HAR o Hetci, cada uno opcionalmente sustituido con 1-3 átomos de halo, 1-4 grupos alquilo c1-6 y 1-2 grupos seleccionados entre grupos CN, NO2, S(O)pRd, halo-alquilo C1-6, alcoxi C1-6 y halo-alcoxi C1-6; y b) Arilo, HAR o Hetci, cada uno opcionalmente sustituido con 1-3 grupos halo y 1-2grupos seleccionados entre CN, NO2, S(O)pRd, alquilo C1-6, alcoxi C1-6, alquenilo C2-6 y arilo, estando dichos alquilo, alcoxi y alquenilo opcionalmente sustituidos con 1-3 átomos de halo, y estando dicho arilo opcionalmente sustituido con 1-3 grupos halo, alquilo C1-6, alcoxi C1-6, halo-alquilo C1-6 y halo-alcoxi C1-6; R3 representa H, alquilo C1-6; 3 grupos R4 están presentes, o-3 de los cuales son grupos alquilo C1-8, alquenilo C2-6, alquinilo C2-6 o alcoxi C1-8, estando dichos grupos opcionalmente sustituidos con (1) 1-5 átomos de halo hasta perhaloalquilo; (2) 1 grupo oxo; (3) 1-2 grupos OH, (4) 1-2 grupos alcoxi C1-10 cada uno opcionalmente sustituido con hasta cinco átomos de halo o a perhaloalcoxi, 1 grupo OH o CO2Ra; (5) 1-2 grupos Arilo, Hetci o HAR, cada uno opcionalmente sustituido de la siguiente manera:(i) 1-5 átomos de halo, (ii) 1 grupo OH, CO2Ra, CN, S(O)pRd, NO2 o C(O)NRbRc; (iii) 1-2 grupos alquilo o alcoxi C1-10; cada uno opcionalmente sustituido co: 1-5 átomos de halo, hasta perhaloalquilo; y 0-1 de los cuales es Arilo opcionalmente sustituido de la siguiente manera: (1) 1-3 átomos de halo; (2) 1-2 grupos OH, CO2Ra, CN o S(O)pRd; (3) 1-3 grupos alquilo C1-8 opcionalmente sustituido con 1-5 grupos halo, y (4) 1-3 grupos alcoxi C1-10, cuya parte alquilo está opcionalmente sustituida con 1-5 grupos halo, y los restantes son átomos de H; R5 representa H, halo, alquilo C1-6, alcoxi C1-6, halo-alquilo C1-6 o halo-alcoxi C1-6; G representa -CHRx- en el que Rx representa H o alquilo C1-8; Ra es H o alquilo C1-10 opcionalmente sustituido con fenilo, OH, O-alquilo C1-6, CO2H, CO2-alquilo C1-6 y 1-3 grupos halo; Rb es H o alquilo C1-10; Rc es H o se selecciona independientemente entre: (a) alquilo C1-10, (b) Arilo o Ar-alquilo C1-6, cada uno opcionalmente sustituido con 1-5 halos y 1-3 miembros seleccionados entre el grupo constituido por: CN, OH, alquilo C1-10 y O-alquilo C1-10, estando además dichos alquilo y alcoxi opcionalmente sustituidos con 1-5 grupos halo hasta perhalo; Rd es alquilo C1-10, Arilo o Ar-alquilo C1-10; p es un numero entero seleccionado entre 0, 1 y 2, y Z se selecciona entre CH2CH2CO2Ra, CH2CH(OH)CO2Ra y 5-tetrazolilo.
ARP060104426A 2005-10-13 2006-10-06 Derivados de acil-indol, composiciones farmaceuticas que los contienen y su uso en el tratamiento de la diabetes mellitus tipo 2. AR056684A1 (es)

Applications Claiming Priority (1)

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US72649205P 2005-10-13 2005-10-13

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AR056684A1 true AR056684A1 (es) 2007-10-17

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ID=37806154

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ARP060104426A AR056684A1 (es) 2005-10-13 2006-10-06 Derivados de acil-indol, composiciones farmaceuticas que los contienen y su uso en el tratamiento de la diabetes mellitus tipo 2.

Country Status (11)

Country Link
US (1) US7598398B2 (es)
EP (1) EP1951669A1 (es)
JP (1) JP2009511581A (es)
AR (1) AR056684A1 (es)
AU (1) AU2006303986B2 (es)
CA (1) CA2624007A1 (es)
DO (1) DOP2006000219A (es)
GT (1) GT200600453A (es)
PE (1) PE20070498A1 (es)
TW (1) TW200745031A (es)
WO (1) WO2007047177A1 (es)

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AU2002351730A1 (en) 2001-12-19 2003-06-30 Novo Nordisk A/S Glucagon receptor antagonists/inverse agonists
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WO2007047177A1 (en) 2007-04-26
US7598398B2 (en) 2009-10-06
EP1951669A1 (en) 2008-08-06
JP2009511581A (ja) 2009-03-19
DOP2006000219A (es) 2007-05-15
TW200745031A (en) 2007-12-16
AU2006303986A1 (en) 2007-04-26
GT200600453A (es) 2007-05-04
CA2624007A1 (en) 2007-04-26
AU2006303986B2 (en) 2010-06-24
US20070088071A1 (en) 2007-04-19

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