PE20080890A1 - DERIVADOS DE IMIDAZOLONA E IMIDAZOLIDINONA COMO INHIBIDORES DE LA 11b-HSD1 PARA LA DIABETES - Google Patents

DERIVADOS DE IMIDAZOLONA E IMIDAZOLIDINONA COMO INHIBIDORES DE LA 11b-HSD1 PARA LA DIABETES

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Publication number
PE20080890A1
PE20080890A1 PE2007001408A PE2007001408A PE20080890A1 PE 20080890 A1 PE20080890 A1 PE 20080890A1 PE 2007001408 A PE2007001408 A PE 2007001408A PE 2007001408 A PE2007001408 A PE 2007001408A PE 20080890 A1 PE20080890 A1 PE 20080890A1
Authority
PE
Peru
Prior art keywords
ona
cycloalkyl
hsd1
imidazolone
imidazolidinone
Prior art date
Application number
PE2007001408A
Other languages
English (en)
Inventor
Jean Ackermann
Kurt Amrein
Daniel Hunziker
Bernd Huhn
Alexander V Mayweg
Werner Neidhart
Tadakatsu Takahashi
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20080890A1 publication Critical patent/PE20080890A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/02Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/06Heterocyclic 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
    • C07D233/08Heterocyclic 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
    • C07D233/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/28Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE IMIDAZOLONA E IMIDAZOLIDINONA DE FORMULA (I) DONDE R1 ES BORNILO, ADAMANTILO, METOXIFENILO, DIFLUOROFENILO, TRIFLUOROMETILFENILO, CIANOFENILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON ALQUILO(C1-C8), HALOGENO, HALOALQUILO(C1-C8), ALCOXI(C1-C8), ENTRE OTROS SUSTITUYENTES; R2 ES H, ALQUILO(C1-C8), CICLOALQUILO(C3-C8), PIRIDINILALQUILO, ENTRE OTROS; R3 Y R4 SON CADA UNO H, ALQUILO(C1-C8), CICLOALQUILO(C3-C8), HALOALQUILO(C1-C8), ENTRE OTROS; R5 Y R6 SON CADA UNO H, ISOPROPILO, ISOBUTILO, CICLOALQUILO(C3-C8) O HALOALQUILO(C1-C8). SON COMPUESTOS PREFERIDOS: 1-ADAMANTAN-2-IL-3-BENZIL-1,3-DIHIDRO-IMIDAZOL-2-ONA, 4-ISOBUTIL-1-(2-TRIFLUOROMETIL-FENIL)-IMIDAZOLIDIN-2-ONA, 1-((E)-5-HIDROXI-ADAMANTAN-2-IL)-4-HIDROXIMETIL-3-METIL-IMIDAZOLIDIN-2-ONA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA 11BETA-HIDROXIESTEROIDE DESHIDROGENASA DE TIPO 1 (11BETA-HSD1) SIENDO UTILES EN EL TRATAMIENTO Y PROFILAXIS DE LA DIABETES DE TIPO 2, OBESIDAD, TRANSTORNOS ALIMENTARIOS, DISLIPIDEMIA, HIPERTENSION
PE2007001408A 2006-10-19 2007-10-17 DERIVADOS DE IMIDAZOLONA E IMIDAZOLIDINONA COMO INHIBIDORES DE LA 11b-HSD1 PARA LA DIABETES PE20080890A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20080890A1 true PE20080890A1 (es) 2008-06-28

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PE2007001408A PE20080890A1 (es) 2006-10-19 2007-10-17 DERIVADOS DE IMIDAZOLONA E IMIDAZOLIDINONA COMO INHIBIDORES DE LA 11b-HSD1 PARA LA DIABETES

Country Status (18)

Country Link
US (1) US8129423B2 (es)
EP (2) EP2104665A2 (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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JP5079011B2 (ja) 2012-11-21
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EP2104665A2 (en) 2009-09-30
TW200831088A (en) 2008-08-01
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CN101553474B (zh) 2013-02-27
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AR063332A1 (es) 2009-01-21
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AU2007312391B2 (en) 2012-06-21
KR20090065535A (ko) 2009-06-22
RU2009118488A (ru) 2010-11-27
IL197955A0 (en) 2009-12-24
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