AR063332A1 - Derivados de imidazolona e imidazolidinona como inhibidores de la 11b-hsd1, un proceso de preparacion y una composicion farmaceutica en base al compuesto - Google Patents

Derivados de imidazolona e imidazolidinona como inhibidores de la 11b-hsd1, un proceso de preparacion y una composicion farmaceutica en base al compuesto

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Publication number
AR063332A1
AR063332A1 ARP070104597A ARP070104597A AR063332A1 AR 063332 A1 AR063332 A1 AR 063332A1 AR P070104597 A ARP070104597 A AR P070104597A AR P070104597 A ARP070104597 A AR P070104597A AR 063332 A1 AR063332 A1 AR 063332A1
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AR
Argentina
Prior art keywords
alkyl
haloalkyl
substituted
independently selected
halogen
Prior art date
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ARP070104597A
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English (en)
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Hoffmann La Roche
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Publication of AR063332A1 publication Critical patent/AR063332A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/06—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/06—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
    • C07D233/08—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms
    • C07D233/10—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Nutrition Science (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Estos compuestos se pueden emplear como medicamentos para el tratamiento de la diabetes, dislipitemias, obesidad e hipertension. 1. Los compuestos de formula (1) en la que R1 es a) bornilo, norbornilo, adamantilo o adamantilo sustituido con uno o dos sustituyentes seleccionados independientemente de entre los siguientes: hidroxi, alcoxi, halogeno, alquilo, hidroxialquilo, amino, aminocarbonilo, alcoxicarbonilo, hidroxicarbonilo, alquilcarbonilamino, alquil-S(O)2-amino, haloalquil-S(O)2- amino, alcoxicarbonilamino-S(O)2-amino, amino-S(O)2-amino, hidroxialquilcarbonilamino, aminocarbonilamino y haloalcoxi; b) trifluorometilfenilo, metoxifenilo, haloalcoxifenilo o difluorofenilo, en el que trifluorometilfenilo, haloalcoxifenilo y difluorofenilo se sustituyen opcionalmente con uno o dos sustituyentes seleccionados independientemente de entre los siguientes: alquilo, halogeno, haloalquilo, alcoxi, hidroxi y haloalcoxi; c) trifluorometilfenilalquilo o trifluorometilfenilalquilo sustituidos con uno o dos sustituyentes seleccionados independientemente de entre los siguientes: alquilo, halogeno, haloalquilo, alcoxi, hidroxi y haloalcoxi; d) fenilcicloalquilo o fenilcicloalquilo sustituido con un numero de sustituyentes de uno a tres seleccionados independientemente de entre los siguientes alquilo, halogeno, haloalquilo, alcoxi, hidroxi y haloalcoxi; e) cianofenilo o cianofenilo sustituido con halogeno; o f) dihalofenilo, aminocarbonilfenilo o hidroxifenilo, en el que el aminocarbonilfenilo y el hidroxifenilo se sustituyen opcionalmente con uno o dos sustituyentes seleccionados independientemente de entre los siguientes: alquilo, halogeno, haloalquilo, alcoxi y haloalcoxi; R2 es hidrogeno, alquilo, alquenilo, haloalquilo, piridinilalquilo, cicloalquilo, cicloalquiloalquilo o fenilalquilo, o R2 es piridinilalquilo o fenilalquilo en que ambos están sustituidos con un numero de sustituyentes de uno a tres seleccionados independientemente de entre los siguientes: alquilo, hidroxi, alcoxi, halogeno, haloalquilo y haloalcoxi; uno entre R3 y R4 es hidrogeno, alquilo, cicloalquilo, haloalquilo o no existe y el otro es: a) hidrogeno, alquilo, piridinilo, cicloalquilo, cicloalquilalquilo o haloalquilo; b) fenilo o fenilo sustituido con un numero de sustituyentes de uno a tres seleccionados independientemente de entre los siguientes fluoro, cloro, bromo, haloalquilo, alcoxi, hidroxi, haloalquilo y haloalcoxi; c) fenilalquilo o piridinilalquilo en que el fenilalquilo y el piridinilalquilo se sustituyen opcionalmente con un numero de sustituyentes de uno a tres seleccionados independientemente de entre los siguientes alquilo, halogeno, haloalquilo e hidroxi; d) oxetano u oxetano sustituido con un grupo alquilo; e) naftilo o tetrahidronaftilo; f) fenilalcoxialquilo o fenilalcoxialquilo sustituido con un numero de sustituyentes de uno a tres seleccionados independientemente de entre los siguientes: alquilo y halogeno; g) hidroxialquilo; o h) piridiniloxialquilo o piridiniloxialquilo sustituido con un grupo ciano; o R3 y R4 junto con el átomo de carbono al que están unidos forman un cicloalcano, piperidina, tetrahidropirano, tetrahidrotiopirano, pirrolidina, tetrahidrofurano, indano u oxetano, en el que el cicloalquilo, piperidina, tetrahidropirano, tetrahidrotiopirano, pirrolidina, tetrahidrofurano, indano y oxetano se sustituyen opcionalmente con un numero de sustituyentes de uno a tres seleccionados independientemente de entre los siguientes: alquilo, arilo y arilalquilo; uno de los radicales R5 o R6 es hidrogeno, isopropilo, isobutilo, cicloalquilo o haloalquilo y el otro es hidrogeno o no existe; y las sales y los ésteres farmacéuticamente aceptables de los mismos siempre que el 1,3-dihidro-4-fenil-1-(3-(trifiuorometil)fenil)-2H-imidazol-2-ona se excluya y, en el caso de que uno de los radicales R3 y sea metilo, etilo, n-propilo o n-butilo y el otro sea hidrogeno o no exista, entonces R2 no sea hidrogeno ni metilo.
ARP070104597A 2006-10-19 2007-10-17 Derivados de imidazolona e imidazolidinona como inhibidores de la 11b-hsd1, un proceso de preparacion y una composicion farmaceutica en base al compuesto AR063332A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06122591 2006-10-19

Publications (1)

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AR063332A1 true AR063332A1 (es) 2009-01-21

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ARP070104597A AR063332A1 (es) 2006-10-19 2007-10-17 Derivados de imidazolona e imidazolidinona como inhibidores de la 11b-hsd1, un proceso de preparacion y una composicion farmaceutica en base al compuesto

Country Status (18)

Country Link
US (1) US8129423B2 (es)
EP (2) EP2308851A1 (es)
JP (1) JP5079011B2 (es)
KR (2) KR20110079776A (es)
CN (1) CN101553474B (es)
AR (1) AR063332A1 (es)
AU (1) AU2007312391B2 (es)
BR (1) BRPI0717657A2 (es)
CA (1) CA2666489C (es)
CL (1) CL2007002972A1 (es)
IL (1) IL197955A0 (es)
MX (1) MX2009003939A (es)
NO (1) NO20091548L (es)
PE (1) PE20080890A1 (es)
RU (1) RU2439062C2 (es)
TW (1) TWI339120B (es)
WO (1) WO2008046758A2 (es)
ZA (1) ZA200902638B (es)

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US8129423B2 (en) 2012-03-06
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